[N:1]1[CH:6]=[CH:5][CH:4]=[N:3][C:2]=1[C:7]1[S:8][C:9]([C:16]([OH:18])=O)=[C:10]([C:12]([F:15])([F:14])[F:13])[N:11]=1.Cl[C:20]1[CH:25]=[CH:24][C:23]([CH:26]([N:29]2[CH2:34][CH2:33]C[CH2:31][CH2:30]2)[CH2:27][NH2:28])=[CH:22][CH:21]=1.F[P-](F)(F)(F)(F)F.[N:42]1(O[P+](N(C)C)(N(C)C)N(C)C)[C:46]2C=CC=CC=2N=N1.CCOC(C)=O>C(#N)C.O>[CH3:46][N:42]1[CH2:31][CH2:30][N:29]([C:26]2([CH2:27][NH:28][C:16]([C:9]3[S:8][C:7]([C:2]4[N:1]=[CH:6][CH:5]=[CH:4][N:3]=4)=[N:11][C:10]=3[C:12]([F:13])([F:14])[F:15])=[O:18])[CH2:22][CH2:21][CH2:20][CH2:25][CH2:24][CH2:23]2)[CH2:34][CH2:33]1A mixture of 2-pyrimidin-2-yl-4-trifluoromethyl-thiazole-5-carboxylic acid (15 mg), 2-(4-chloro-phenyl)-2-piperidin-1-yl-ethylamine (15 mg), BOP (25 mg) and TEA (10 mg) in ACN (1 mL) is stirred at RT overnight. EtOAc and water are added to the mixture and the organic layer is separated, washed twice with water and concentrated in vacuo. The residue is purified by PTLC (10% MeOH in methylene chloride) to give the title compound. MS (M+1)=483.21; RT=1.15 min. *IC50.
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